Selective-inhibition of Trypanosomal Triosephosphate Isomerase By a Thiopeptide
(1992) Angewandte Chemie: International Edition in English — Vol. 31, n° 3, p. 328-330 (1992)
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- Abstract
- One approach to conquering sleeping sickness is the selective inhibition of trypanosomal triosephosphate isomerase, a key enzyme in the pathogen's metabolism, with cyclic hexapeptides. The thionylation of the Phe5-Phe6 amide bond of the cyclic hexapeptide cyclo(Gly1-Pro2-Phe3-Val4-Phe5-Phe6) is a minor modification, but effects a total rearrangement of the intramolecular hydrogen bonds which causes a drastic improvement of inhibitoric activity-maximum effect from minimum chemistry!
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Kessler, H., Matter, H., Geyer, A., Diehl, HJ., Kock, M., Kurz, G., Opperdoes, F., Callens, M., & Wierenga, RK. (1992). Selective-inhibition of Trypanosomal Triosephosphate Isomerase By a Thiopeptide. Angewandte Chemie: International Edition in English, 31(3), 328-330. https://doi.org/10.1002/anie.199203281 (Original work published 1992)